Delivery system having stabilized ascorbic acid and other actives

ABSTRACT

The present invention provides for a formulation manufactured by a process comprising: admixing at least one elastomer with a first dispersant to form a gel; admixing a second dispersant with the gel; and admixing at least one active, such as ascorbic acid, with the gel to form a delivery system with an active in the formulation retains its stability, functionality and aesthetics.

BACKGROUND OF INVENTION

1. Field of Invention

The present invention relates a delivery system with actives such asascorbic acid that retain their stability, functionality and aesthetics.In particular, a formulation and related method of manufacturecomprising: at least one elastomer; a first dispersant; a seconddispersant and at least one active wherein the formulation forms adelivery system wherein the active in the formulation retains itsstability, functionality and aesthetics.

2. Description of Related Art

The prior art shows that the most crucial problem with any water solubleantioxidant, such as ascorbic acid, is its stability in a formulation.In addition, these antioxidants or actives are crystalline or powder,and would feel like “sand” when formulated into a skin care or cosmeticproduct. Furthermore, the prior arts' teachings of incorporating theseactives into anhydrous systems do not solve the problem. The “feel” ofthe skin care or cosmetic products using the anhydrous system isundesirable.

The present invention provides for a delivery system wherein the watersoluble antioxidant retains its stability, functionality and aesthetics.

SUMMARY OF INVENTION

In one embodiment, the present invention provides for a formulationcomprising: at least one elastomer; a first dispersant; a seconddispersant and at least one active wherein the formulation forms adelivery system wherein the active in the formulation retains itsstability, functionality and aesthetics.

In another embodiment, the elastomer is selected from a group consistingessentially of Dimethicone Copolymers in Dimethicone, VinyldimethiconeCopolymers in Dimethicone, Dimethicone crosspolymers in Dimethicone,Vinyldimethicone crosspolymers in Dimethicone, Silicone and combinationand mixtures thereof. For purposes of this invention, the term“elastomer” is defined as any natural or synthetic material, includingpolymers, that is able to resume its original shape when a deformingforce is removed.

In yet another embodiment, the first dispersant is selected from a groupconsisting essentially of Cyclomethicone, Isododecane, Hydrocarbons,Esters, Dimethicones, petrolatum, Cyclopentasiloxane, and combinationand mixtures thereof.

In still another embodiment, the second dispersant is selected from agroup consisting essentially of Dimethicone, Cyclomethicones,Hydrocarbons, Esters, and combination and mixtures thereof. For purposesof this invention, the term “dispersant” is defined as a liquid or gasadded to a mixture to promote dispersion or maintain dispersed particlesin suspension and also includes any material that is able to gel theelastomer dispersed in it while keeping its structure and stability overtime.

In still yet another embodiment, the active is selected from a groupconsisting essentially of Ascorbic Acid, Epigallo Catechin Gallate(EGCG), Hydroquinone, Ubiquinone, Ubiquinol, Ferrulic Acid, Lipoic acid,and combination and mixtures thereof.

In a further embodiment, the formulation can be used as a productselected from a group consisting of skin care products, cosmetics,cosmeceuticals, pharmaceuticals and nutriceuticals. In another furtherembodiment, the formulation can be combined with other components andingredients to form a product selected from a group consisting of skincare products, cosmetics, cosmeceuticals, pharmaceuticals andnutriceuticals.

In yet a further embodiment, the formulation further comprises anactivator selected from a group consisting essentially of Water,Glycerin, Glycols, Polyols, Polyglutamic Acid, Hyaluronic Acid, andcombination and mixtures thereof.

In still a further embodiment, the formulation further comprises atleast one anhydrous system such as steardimonium hectorite anddisteardimonium hectorite with organic sunscreens. For purposes of thisinvention, the term “anhydrous” is defined as any non-aqueous (no water)or limited water containing formulation or composition.

In still yet a further embodiment, the second dispersant has a viscosityfrom about 0.65 to about 350 centistoke.

In another embodiment, the present invention provides for a formulationmanufactured by a process comprising: admixing at least one elastomerwith a first dispersant to form a gel; admixing a second dispersant withthe gel; and admixing at least one active with the gel to form adelivery system with an active in the formulation retains its stability,functionality and aesthetics.

In yet another further embodiment, the second dispersant has a viscosityfrom about 0.65 to about 20 centistoke.

In yet another further embodiment, the process further comprisesadmixing at least one sunscreen formulation.

In still another further embodiment, the present invention relates to aformulation containing ascorbic acid, and the formulation comprises: atleast one elastomer; a first dispersant; a silicone and ascorbic acidwherein the formulation forms a delivery system wherein the ascorbicacid in the formulation retains its stability, functionality andaesthetics.

In still yet another further embodiment, the present invention providesfor a formulation manufactured by a process comprising: admixing atleast one elastomer with a first dispersant to form a gel; admixing asilicone with the gel; and admixing ascorbic acid with the gel to form adelivery system with an active in the formulation retains its stability,functionality and aesthetics.

In another embodiment, the process further comprises admixing at leastone activator selected from a group consisting essentially of Water,Glycerin, Glycols, Polyols, Polyglutamic Acid, Hyaluronic Acid, andcombination and mixtures thereof.

DETAILED DESCRIPTION OF THE INVENTION

As required, detailed embodiments of the present invention are disclosedherein; it is to be understood that the disclosed embodiments are merelyexemplary of the invention that may be embodied in various forms.Therefore, specific structural and functional details disclosed hereinare not to be interpreted as limits, but merely as a basis for teachingone skilled in the art to employ the present invention. The specificexamples below will enable the invention to be better understood.However, they are given merely by way of guidance and do not imply anylimitation.

In one embodiment, the focus of the present invention is stabilizing,inherently, unstable water-soluble anti-oxidants or actives such asAscorbic Acid (AA), Epigallocatechin Gallate (EGCG), and N-acetylglucosamine (NAG). These actives help to protect the skin when appliedtopically, by reducing the action of free radicals that can cause harmto cells. When the molecules are dissolved in water they also are opento oxidation, before they can be applied to skin. When the molecules arein their slid form, they are very stable. One option is to dispersethese actives in an essentially anhydrous vehicle, however, the endproduct is not aesthetically viable for commercial purposes. The activesare crystalline or powder, and would feel like “sand” when formulatedinto a skin care or cosmetic product and therefore, undesirable toconsumers.

In another embodiment, the present invention provides for a solutionusing gels. The selection of the gelling agent is critical. If thevehicle is too thin, the materials will sink to the bottom and theformula will not be homogeneous, and will not be able to deliver properdoses to the skin. If the vehicle is too thick, it will not apply evenlyand the consumer/end user will not like the “feel”.

In a further embodiment, using a gel having a cream-like consistency isoptimal. It allows the consumer to apply and enjoy the comfort andbenefit of the therapy. In another embodiment, the presently claimedinvention uses Elastomer technology to achieve the desired results.Dimethicon/vinyldimethicone crosspolymers have been used in cosmetics tocreate great texture and feel. Interestingly, when one of thesemolecules is added to the different elastomer gels, the combination isstable but is aesthetically undesirable because you can feel thescratchiness of the dispersed materials. Therefore the right dispersingagents must be used to not only gel the elastomer, but to enable theactive materials to blend into the base homogeneously.

The present invention has shown that using Isododecane andCyclopetasiloxane, and Dimethicone 5 cps provides for desired results.Although we recognize that there are other materials that could have asimilar effect, to achieve the overall viscosity and texture for afinished formulation that has extraordinary aesthetics a seconddispersant is used to fine tune the right consistency. Elastomers aresilicone rubbers that have been used in many industries. The finishedformula we have is cosmetically commercial and viable. It efficientlystabilizes the actives until they reach the skin. The water proof filmthat is left on the skin after it is applied, not only is silky smoothand desirable but helps to aid the penetration and keep the active inplace, until it can be absorbed.

The following examples are set forth below:

EXAMPLE 1 Vitamin C Formulation

Phase A is weighed in kettle equipped with a high speed agitation. PhaseB is then added to Phase A and mixed until homogeneous. Phase C is thenslowly admixed with Phase AB and then mixed on very high speed. Theingredients and % of each ingredient in the composition is set forthbelow in Table 1.

TABLE 1 Phase: Ingredients: INCI % A IDS-5 Cyclopentasiloxane & 65.00Polysilicone-11 & Isododecane B DC 200 5 cst Dimethicone 15.00 C VitaminC Ascorbic Acid 20.00 100.00

EXAMPLE 2 Vitamin C, N-Acetyl D-Glucosamine & Green Tea ExtractFormulation

Phase A is weighed in kettle equipped with a high speed agitation. PhaseB is then added to Phase A and mixed until homogeneous. Phase C is thenslowly admixed with Phase AB and then mixed on very high speed. Theingredients and % of each ingredient in the composition is set forthbelow in Table 2.

TABLE 2 Phase: Ingredients: INCI % A IDS-5 Cyclopentasiloxane & 59.00Polysilicone-11 B DC 200 5 cst Dimethicone 15.00 C Vitamin C AscorbicAcid 20.00 N-Acetyl D-Glucosamine N-Acetyl D-Glucosamine 5.00 Green TeaExtract Epigallo Catechin Gallate 1.00 (EGCG) 100.00

EXAMPLE 3 Green Tea Extract Formulation

Phase A is weighed in kettle equipped with a high speed agitation. PhaseB is then added to Phase A and mixed until homogeneous. Phase C is thenslowly admixed with Phase AB and then mixed on very high speed. Theingredients and % of each ingredient in the composition is set forthbelow in Table 3.

TABLE 3 Phase: Ingredients: INCI % A IDS-5 Cyclopentasiloxane & 93.00Polysilicone-11 B DC 200 5 cst Dimethicone 5.00 C Green Tea ExtractEpigallo Catechin Gallate 2.00 (EGCG) 100.00

EXAMPLE 4 N-Acetyl D-Glucosamine Formulation

Phase A is weighed in kettle equipped with a high speed agitation. PhaseB is then added to Phase A and mixed until homogeneous. Phase C is thenslowly admixed with Phase AB and then mixed on very high speed. Theingredients and % of each ingredient in the composition is set forthbelow in Table 4.

TABLE 4 Phase: Ingredients: INCI % A IDS-5 Cyclopentasiloxane & 82.00Polysilicone-11 B DC 200 5 cst Dimethicone 10.00 C N-AcetylD-Glucosamine N-Acetyl D-Glucosamine 8.00 100.00

Stability tests were also conducted over a six month period and thetests results showed no deterioration of the actives. The stabilitytests are set for the below in Table 5:

ICC STABILIZED ACTIVE STABILITY DATA Initial 24 Hour Month 1 Month 2Month 3 Month 6 CONTROL VITAMIN C 25° C. Water White Water white YellowDk. Yellow/OJ Dk. Yellow/OJ Dk. Yellow/OJ 50° C. Water White Sl. YellowDk. Yellow Deep Orange Deep Orange Deep Orange VITAMIN C J116.01 25° C.White Cream White Cream White Cream White Cream White Cream White Cream50° C. White Cream White Cream White Cream White Cream White Cream WhiteCream Vitamin C Anhydrous System J116.02 25° C. Sl. Pink Beige Sl. PinkBeige Sl. Pink Beige Sl. Pink Beige Sl. Pink Beige Sl. Pink Beige 50° C.Sl. Pink Beige Sl. Pink Beige Sl. Pink Beige Sl. Pink Beige Sl. PinkBeige Sl. Pink Beige CONTROL EGCG 25° C. Slight Brown Slight Brown DarkBrown Dark Brown/Red Dark Brown/Red Dark Brown/Red 50° C. Slight BrownDk. Brown Dark Brown/Red Dark Brown/Red Dark Brown/Red Dark Brown/RedEGCG Anhydrous System J116.03 25° C. Sl. Pink Beige Sl. Pink Beige Sl.Pink Beige Sl. Pink Beige Sl. Pink Beige Sl. Pink Beige 50° C. Sl. PinkBeige Sl. Pink Beige Sl. Pink Beige Sl. Pink Beige Sl. Pink Beige Sl.Pink Beige N-Acetyl D-Glucosamine Anhydrous System J116.04 25° C. WhiteCream White Cream White Cream White Cream White Cream White Cream 50° C.White Cream White Cream White Cream White Cream White Cream White Cream*Color Only due to natural coloration to EGCG and indicates nodegredation or discoloration of formula

The present invention is not limited to the above Examples and Tables.Numerous modifications and variations of the present invention arepossible in light of the above teachings. It is therefore to beunderstood that within the scope of the attendant claims attachedhereto, this invention may be practiced other than as specificallydisclosed herein.

What is claimed is:
 1. A formulation consisting of: at least oneelastomer selected from a group consisting of Dimethicone Copolymers inDimethicone, Vinyldimethicone Copolymers in Dimethicone, Dimethiconecrosspolymers in Dimethicone, Vinyldimethicone crosspolymers inDimethicone, Silicone, and combination and mixtures thereof; a firstdispersant selected from a group consisting of Cyclomethicone,Isododecane, Hydrocarbons, Esters, Dimethicones, petrolatum,Cyclopentasiloxane, and combination and mixtures thereof; a seconddispersant selected from a group consisting of Dimethicone,Cyclomethicones, Hydrocarbons, Esters, and combination and mixturesthereof; at least one active selected from a group consisting ofAscorbic Acid, Epigallo Catechin Gallate (EGCG), Hydroquinone,Ubiquinone, Ubiquinol, Ferrulic Acid, Lipoic acid, and combination andmixtures thereof; an activator selected from a group consisting ofWater, Glycerin, Glycols, Polyols, Polyglutamic Acid, Hyaluronic Acid,and combination and mixtures thereof; and an anhydrous system which isselected from a group consisting of steardimonium hectorite,disteardimonium hectorite, and combination and mixtures thereof, whereinsaid formulation forms a delivery system wherein said active in saidformulation retains its stability, functionality and aesthetics.
 2. Theformulation of claim 1 wherein said formulation can be used as a productselected from a group consisting of skin care products, cosmetics,cosmeceuticals, pharmaceuticals and nutriceuticals.
 3. The formulationof claim 1 wherein said second dispersant has a viscosity from about0.65 to about 350 centistoke at 25 degrees Celsius.
 4. A process formanufacturing a formulation, said process consisting of: admixing atleast one elastomer with a first dispersant to form a gel, saidelastomer is selected from a group consisting of Dimethicone Copolymersin Dimethicone, Vinyldimethicone Copolymers in Dimethicone, Dimethiconecrosspolymers in Dimethicone, Vinyldimethicone crosspolymers inDimethicone, Silicone, and combination and mixtures thereof, said firstdispersant is selected from a group consisting of Cyclomethicone,Isododecane, Hydrocarbons, Esters, Dimethicones, petrolatum,Cyclopentasiloxane, and combination and mixtures thereof; admixing asecond dispersant with said gel, second dispersant is selected from agroup consisting of Dimethicone, Cyclomethicones, Hydrocarbons, Esters,and combination and mixtures thereof, admixing at least one active withsaid gel to form a delivery system wherein said active in saidformulation retains its stability, functionality and aesthetics, saidactive is selected from a group consisting of Ascorbic Acid, EpigalloCatechin Gallate (EGCG), Hydroquinone, Ubiquinone, Ubiquinol, FerrulicAcid, Lipoic acid, and combination and mixtures thereof; admixing atleast one activator with said gel wherein said activator is selectedfrom a group consisting of Water, Glycerin, Glycols, Polyols,Polyglutamic Acid, Hyaluronic Acid, and combination and mixtures thereofadmixing an anhydrous system with said gel wherein said anhydrous systemis selected from a group consisting of steardimonium hectorite,disteardimonium hectorite, and combination and mixtures thereof; andadmixing at least one organic sunscreen.
 5. The process of claim 4wherein said formulation can be used as a product selected from a groupconsisting of skin care products, cosmetics, cosmeceuticals,pharmaceuticals and nutriceuticals.
 6. The formulation of claim 4wherein said second dispersant has a viscosity from about 0.65 to about20 centistoke at 25 degrees Celsius.
 7. A formulation consisting of: atleast one elastomer; a first dispersant selected from a group consistingof Dimethicone Copolymers in Dimethicone, Vinyldimethicone Copolymers inDimethicone, Dimethicone crosspolymers in Dimethicone, Vinyldimethiconecrosspolymers in Dimethicone, Silicone and combination and mixturesthereof; a second dispersant selected from a group consisting ofDimethicone, Cyclomethicones, Hydrocarbons, Esters, and combination andmixtures thereof; an active, wherein said active is selected from agroup consisting of Ascorbic Acid, Epigallo Catechin Gallate (EGCG),Hydroquinone, Ubiquinone, Ubiquinol, Ferrulic Acid, Lipoic acid, andcombination and mixtures thereof, wherein said formulation forms adelivery system wherein said active in said formulation retains itsstability, functionality and aesthetics.
 8. A process for manufacturinga formulation, said process consisting of: admixing at least oneelastomer with a first dispersant to form a gel, said elastomer isselected from a group consisting of Dimethicone Copolymers inDimethicone, Vinyldimethicone Copolymers in Dimethicone, Dimethiconecrosspolymers in Dimethicone, Vinyldimethicone crosspolymers inDimethicone, Silicone, and combination and mixtures thereof, said firstdispersant is selected from a group consisting of Cyclomethicone,Isododecane, Hydrocarbons, Esters, Dimethicones, petrolatum,Cyclopentasiloxane, and combination and mixtures thereof; admixing asilicone with said gel; admixing ascorbic acid with said gel to form adelivery system wherein said ascorbic acid in said formulation retainsits stability, functionality and aesthetics; and admixing an anhydroussystem with said gel wherein said anhydrous system is selected from agroup consisting of steardimonium hectorite, disteardimonium hectorite,and combination and mixtures thereof.